| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
Cell lines | T cells |
Preparation Method | Purified WT or Sirt-1–/– T cells were labeled with CFSE and cocultured with T-cell-depleted splenocytes as APCs from BALB/c mice for 5 days in the presence of either dimethyl sulfoxide or EX 527 (10 μg/mL). Cells were restimulated with phorbol 12-myristate 13-acetate and ionomycin for cytokine measurement. |
Reaction Conditions | 10 μg/mL, 5 days |
Applications | T cells with allogeneic antigen-presenting cells (APCs) in vitro, and found that EX 527 significantly reduced CD4 T-cell proliferation and IFN-γ production to a comparable level of Sirt-1–/– T cells. |
Animal models | Male ZDF rats (body weight 300 ± 25 g) |
Preparation Method | EX-527 (5 μg/kg, twice weekly) was administered intraperitoneally (i.p.) to HFD-fed rats for ten weeks. The normal diet-fed rats received diets which were devoid of fats. Glucose levels were determined by using a glucometer. |
Dosage form | 5 μg/kg, i.p. |
Applications | Two weeks after HFD-feeding, blood glucose concentration was increased significantly in HFD fed rats than that of normal diet-fed rats. However, fasting blood glucose level was dramatically decreased in the HFD-fed rats following EX 527 treatment. |
| 文献引用 | |
| 产品描述 | EX 527, as a SIRT1-selective inhibitor, inhibits Sirt1 ~100-fold more potently than Sirt2 and Sirt3 and has no effect on Sirt5′s deacetylation activit.The IC50 values for Sirt1 and Sirt3 are 0.09 ± 0.03 μM and 22.4 ± 2.7 μM, respectively. Sir2Tm was also efficiently inhibited by Ex-527 with IC50 of 0.9 ± 0.3 μM.[1] In vitro experiment it shown that cell viability significantly increased and cell death decreased in cancer cells with SIRT1 silencing or EX 527 (10 μM) treatment compared with the control after exposure to RSL3 or sulfasalazine.[2]In vitro, treatment with 1 μM EX-527 decreased colony formation of ovarian carcinoma cells, with or without overexpression of SIRT172. However, at 600 nM, EX-527 suppressed cell migration and inhibited the occurrence of epithelial–mesenchymal transition (EMT) in chemotherapy resistant oesophageal cancer cells.[4]In vitro experiment it indicated that SIRT 1 inhibition by EX 527 (10 μM) elevated ROS production. SIRT1 and PGC-1α levels were dramatically decreased.[6] In vivo efficacy test indicated that pharmacological blockade of Sirt-1 with 2 mg/kg EX 527/mouse/day daily for 3 weeks alleviated GVHD without impairing T-cell-mediated GVL activity.[3]In vivo efficacy study demonstrated that treatment with 5 mg/kg EX 527 intraperitoneally in C57BL/6J mice abolished the protective effects of melatonin.[4]In vivo, the data indicated that LPS-induced intrapulmonary inflammation and LPS-induced elevation of 4E-BP1 phosphorylation were attenuated by EX 527 (10 mg/kg, i.p.).[5] References: |
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